Sunitinib

製品コードS7781 別名:SU11248

Sunitinib化学構造

分子量(MW):398.47

Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

サイズ 価格(税別)  
JPY 18100
JPY 34700
最寄りの販売代理店を探す

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください:[email protected]

バルク問合せ

文献中Selleckの製品使用例(58)

製品安全説明書

PDGFR阻害剤の選択性比較

生物活性

製品説明 Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
ターゲット
FLT3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
体外試験

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SW756 cell NWW5ZnR7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn7KTY5pcWKrdHnvckBw\iCqdX3hckBUXzd3NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlE{PTFizszN NGPmPIlUSU6JRWK=
human EoL-1-cell cell MlvYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKGi3bXHuJGVwVC1zLXPlcIwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjZ2ZT2wOi=> MmToV2FPT0WU
human MV-4-11 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX;Jcohq[mm2aX;uJI9nKGi3bXHuJG1XNTRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI4OiCwTR?= NGmycYdUSU6JRWK=
human MV411 cells MnLBVJJwdGmoZYLheIlwdiCjc4PhfS=> M{TvWVQ5KGh? Mo\4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPVkSxNUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDpZ|UxRTNibl2= MlrmNlQ6ODR7NkG=
3T3 cells M17GOWZ2dmO2aX;uJIF{e2G7 MnjPTY5pcWKrdHnvckBw\iCSRFfGMYlv\HWlZXSgRpJlXSCrbnPvdpBwemG2aX;uJIlvKDOWMzDj[YxteyC5aYToJFAvOSViYn;2bY5mKHOncoXtJIFt[nWvaX6sJGlEPTB;NzDuUS=> MkfhNVI3PDZyMUm=
HEK293 cells NWnET4lRTnWwY4Tpc44h[XO|YYm= NWHLe4xQSmmwZHnu[{Bi\m[rbnn0fUB1dyCITGSzJINifGGueYTpZ{Bld22jaX6g[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDifUBkd22yZYTpeIl3\SCkaX7kbY5oKGG|c3H5MEBM\D1yLkS3JI5O NHTqdokyQTd3NEG5PS=>
human MDA-MB-435 cells MnzwR5l1d3SxeHnjxsBie3OjeR?= NWraTYVDOiCq M{[zb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGlEPTB;OT63JI5O MXqyOFg6ODZ3Mh?=
human RS4-11 cells M16wZmZ2dmO2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKE[OVEOgZZV1d3Cqb4PwbI9zgWyjdHnvckBqdiCqdX3hckBTWzRvMUGgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkh\WynY4Tyc4Np\W2rbIXtbY5me2OnbnPlJIF{e2G7LDDJR|UxRTlwOTDuUS=> Mn3tNVk3PTR2MEi=
HUVEC NYnEfoJwS3m2b4TvfIlkyqCjc4PhfS=> MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBJXV[HQzygTWM2OD1zMT64JI5O NV3xRmhKOjR6OUC2OVI>
human Kasumi-1 cells M2j5OWZ2dmO2aX;uJIF{e2G7 MlfwTY5pcWKrdHnvckBw\iClLVvpeEBifXSxcHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEujc4XtbU0yKGOnbHzzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrczygTWM2OD1zNTDuUS=> MW[yNFg{OzB|OR?=
human NOS-1 cell M4PXVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlvyTY5pcWKrdHnvckBw\iCqdX3hckBPV1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlMhdk1? MUjTRW5ITVJ?
mouse triple negative 4T1 cells Mn7yR5l1d3SxeHnjxsBie3OjeR?= MmrhR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgeJJqeGynIH7l[4F1cX[nIETUNUBk\WyuczygTWM2OD1zNjDuUS=> MnizNlQ5QTB4NUK=
human RS4-11 cells NXjZXpVmTnWwY4Tpc44h[XO|YYm= MoD2TY5pcWKrdHnvckBw\iCITGSzJIF2fG:yaH;zdIhwenmuYYTpc44hcW5iaIXtZY4hWlN2LUGxJINmdGy|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF0yPiCwTR?= M{PLTlIxQDN|MEO5
human MOLM13 cells MVrDfZRwfG:6aXRCpIF{e2G7 NFjwZ21EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOV0yPMUOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yPy55IH7N MYSyOVA5QThzMB?=
human U251 cells MULGeY5kfGmxbjDhd5NigQ>? NEHMO|hKdmirYnn0bY9vKG:oIG\FS2ZTOiCrbjDoeY1idiCXMkWxJINmdGy|IHL5JJBpd3OyaH;0fZJwe2mwZTDFUGlUSSxiSVO1NF0yQC57IH7N MV:yOFkxODh4NR?=
NIH3T3 cells MX3GeY5kfGmxbjDhd5NigQ>? NWm4VmpmOSCq MnTzTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiaIXtZY4hU0SUIHvpcoF{\SCneIDy[ZN{\WRiaX6gUmlJO1R|IHPlcIx{KHerdHigOEB2VSCEaX;0bY4uSWi6LVHFSWV[Tk[ORlGtZY1q\GViYYSgZY1jcWWwdDD0[Y1x\XKjdIXy[UBnd3JiMTDodi=> MWCxOlE3OjByOB?=
MDA-MB-231 cells MonSR5l1d3SxeHnjxsBie3OjeR?= NHPJVolEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckB1emmybHWgcoVo[XSrdnWgUWRCNU2ELUKzNUBk\WyuczygTWM2OD1{Mj6zJI5O NGLTNIIzPDh7ME[1Ni=>
MCF7 cells NX\0OohJS3m2b4TvfIlkyqCjc4PhfS=> MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDFVk1xd3OrdHn2[UBOS0Z5IHPlcIx{NCCLQ{WwQVI4NjFibl2= MU[yOFg6ODZ3Mh?=
human CGTH-W-1 cell NXrVTJFuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUjOPJhrUW6qaXLpeIlwdiCxZjDoeY1idiCFR2TIMXcuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNyLkm0JI5O MlzaV2FPT0WU
human MONO-MAC-6 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWDQUnpLUW6qaXLpeIlwdiCxZjDoeY1idiCPT17PMW1CSy14IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{OuPEBvVQ>? M3HoW3NCVkeHUh?=
human HL60 cells MVTDfZRwfG:6aXRCpIF{e2G7 NGTNfJk1QCCq Mn7ER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUO2Mlghdk1? M37JPVI2ODh7OEGw
human TT cells Mlj6VJJwdGmoZYLheIlwdiCjc4PhfS=> MofKO|IhcA>? MnjVRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWVDDj[YxteyCycnX0doVifGWmIH\vdkA4OiCqcoOg[o9tdG:5ZXSgZpkh[2:vcH;1coQuf2G|aH;1eEBu\WG|dYLl[EBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSwJI5O NEnh[4IzPDlyNEm2NS=>
human THP1 cells MnPuR5l1d3SxeHnjxsBie3OjeR?= MlztOFghcA>? M2HiRmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHRJWDFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20OU44KG6P MXiyOVA5QThzMB?=
3T3 cells NX3QWoNjTnWwY4Tpc44h[XO|YYm= Ml7sTY5pcWKrdHnvckBw\iCYYYPjeYxieiCnbnTveIhmdGmjbDDndo94fGhiZnHjeI9zKHKnY3XweI9zKGmwIEPUN{Bk\WyuczygTWM2OD13MDDuUS=> NXPB[ollOTJ4NE[wNVk>
human ALL-PO cell NISxNHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIr2VXRKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVc6Njh7IH7N MV;TRW5ITVJ?
human SH-SY5Y cells MX7GeY5kfGmxbjDhd5NigQ>? NF3jR|NKdmirYnn0bY9vKG:oIGDES2ZT[mW2YTDpckBpfW2jbjDTTE1UYTW\IHPlcIx{KGK7IIDoc5NxcG:2eYLvd4lv\SCHTFnTRUBie3OjeTygTWM2OD16Mz6xJI5O NWi0SnZpOjR6OUC2OVI>
human U251 cells NYXLWG5{TnWwY4Tpc44h[XO|YYm= MYm2NEBucW6| M1T1RmlvcGmkaYTpc44hd2ZiUFTHSnIu[mW2YTDpckBpfW2jbjDVNlUyKGOnbHzzJINwdXCxdX7kJJBz\XS{ZXH0[YQh\m:{IE[wJI1qdiCkZX\vdoUhWESJRj3CRkB{fGmvdXzheIlwdiCob4KgNVAhdWmwczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FiY4n0c4Jtd3RibXX0bI9lNCCLQ{WwQVg{NjFibl2= NXr1b21YOjV6OEK1NVk>
human NKM-1 cell NHnPXnFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MorXTY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm4MlUzKG6P MnPPV2FPT0WU
human HAEC cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 NGHTUoU4OiCq NFjqcZpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjBSWMh[2WubIOg[ZhxemW|c3nu[{BXTUeIUjDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMTFOwG0> NHTHenQzOjR2NE[3PS=>
HUVEC cell M2jlR2Z2dmO2aX;uJIF{e2G7 MkfiNlQhcA>? MnjnTY5pcWKrdHnvckBw\iCYRVfGMWEhcW6mdXPl[EBJXV[HQzDj[YxtKHOycn;1eIlv\yCjZoTldkAzPCCqcoOgZpkh[W6paX;n[Y5me2m|IHHzd4F6NCCLQ{WwQVAvOTJizszN MWWyNVc1OTJ2OR?=
human A431 cells MljQSpVv[3Srb36gZZN{[Xl? NVLNcnRzPjBibXnudy=> NHu5NoVKdmirYnn0bY9vKG:oIFXHSnIhcW5iaIXtZY4hSTR|MTDj[YxteyClb33wc5Vv\CCycnX0doVifGWmIH\vdkA3OCCvaX6gZoVnd3KnIFXHSkB{fGmvdXzheIlwdiCob4KgNVAhdWmwczDifUBxcG:|cHjveJlzd3OrbnWgSWxKW0FiY4n0c4Jtd3RibXX0bI9lNCCLQ{WwQVE4Oi5zIH7N M{\nR|I2QDh{NUG5
Sf9 cells MmT4SpVv[3Srb36gZZN{[Xl? NUPweo9PUW6qaXLpeIlwdiCxZjDHV3QufGGpZ3XkJHZGT0[UIHX4dJJme3OnZDDpckBU\jliY3XscJMtKEmFNUC9NE4yQDVizszN M2TScFE6QDV2MEWx
human HT-29 cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 NVn6SoZUPzJiaB?= MlXzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDlfJBz\XO|aX7nJHZGT0[UIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XoxvJygTWM2OD1yLkOzJO69VQ>? NHjmZYozOjR2NE[3PS=>
human KM12 cell M4OxS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkO1NFE1KM7:TR?= M33hd3NCVkeHUh?=
human TE-15 cell NFnTWo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MljpTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVA4PjFizszN NH\ueHBUSU6JRWK=
human 697 cell M1uySGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NELkTVJKdmirYnn0bY9vKG:oIHj1cYFvKDZ7NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOlE1OjVizszN NVjYRmY1W0GQR1XS
human CAKI-1 cells NHziNG1Rem:uaX\ldoF1cW:wIHHzd4F6 NIjoSJlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPBT2kuOSClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOlMh|ryP M1rZelIzPTZyNkK3
human MOLT-16 cell NVz0RYRYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnXMTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43OzF|MjFOwG0> NYHrUYprW0GQR1XS
human GB-1 cell M2XjNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jWNWlvcGmkaYTpc44hd2ZiaIXtZY4hT0JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|ExOjNizszN NH7hc5NUSU6JRWK=
human TE-12 cell M4W5Xmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkfpTY5pcWKrdHnvckBw\iCqdX3hckBVTS1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPFA1PTVizszN MlSzV2FPT0WU
human NCI-H3122 cells NH3KPXpRem:uaX\ldoF1cW:wIHHzd4F6 NWjEWXZOPzJiaB?= MnTERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMyOjJiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlg{KM7:TR?= NWTNUHp5OjR7MES5OlE>
human ES6 cell M170TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{XLdGlvcGmkaYTpc44hd2ZiaIXtZY4hTVN4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD65PFExPiEQvF2= NHP5[4NUSU6JRWK=
human NCI-H526 cells NXPkbHdnWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHjxelA4OiCq M17aXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg2OjZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlAyKM7:TR?= M2XySFI1QTB2OU[x
human LC-2-ad cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWDkTIRjUW6qaXLpeIlwdiCxZjDoeY1idiCOQz2yMYFlKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5zMUSwO{DPxE1? M1LROnNCVkeHUh?=
human BL-70 cell MoPXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUCzcJlRUW6qaXLpeIlwdiCxZjDoeY1idiCETD23NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOTF6NE[g{txO MXHTRW5ITVJ?
human ETK-1 cell NGPZPYVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnnd4lvUW6qaXLpeIlwdiCxZjDoeY1idiCHVFutNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjh3ODFOwG0> M3HpXnNCVkeHUh?=
human SW620 cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 M170blQ5KGh? MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNkKwJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5|IN88US=> NI\UVWszOjV4ME[yOy=>
IM9 cells MkPlR5l1d3SxeHnjxsBie3OjeR?= MlrzR5l1d3SxeHnjbZR6KGGpYXnud5QhUG:vbzDzZZBq\W6|IDjoeY1idiliSV25JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjN3IN88US=> NI\rPINUSU6JRWK=
human A4-Fuk cell M2HyOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWrZS24zUW6qaXLpeIlwdiCxZjDoeY1idiCDND3GeYsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTFwM{SxOFEh|ryP NH7n[IpUSU6JRWK=
human SR cell M2P5OGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnO5TY5pcWKrdHnvckBw\iCqdX3hckBUWiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNUS1O|Ih|ryP Mn3vV2FPT0WU
human A3-KAW cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHvVfXNKdmirYnn0bY9vKG:oIHj1cYFvKEF|LVvBW{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCrY{WwQVEvPjJ3NE[g{txO MnHsV2FPT0WU
human KS-1 cell NXjsb2lZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIjtbllKdmirYnn0bY9vKG:oIHj1cYFvKEuVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY6OjR5IN88US=> MVfTRW5ITVJ?
human CTV-1 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJGNVXi1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63Nlc2OSEQvF2= M4e1Z3NCVkeHUh?=
human LB1047-RCC cell NVPSZZVGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUHsS4JpUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64NVYzPCEQvF2= M{XnT3NCVkeHUh?=
human MEG-01 cell NXnTWY94T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXXvVlBHUW6qaXLpeIlwdiCxZjDoeY1idiCPRVetNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjh|NU[zJO69VQ>? MU\TRW5ITVJ?
human TE-11 cell NHjYUnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWLJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTFzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT64N|k5PSEQvF2= M3nqenNCVkeHUh?=
human CMK cell NVnu[3FRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXjVPZZIUW6qaXLpeIlwdiCxZjDoeY1idiCFTVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlk2PTF5IN88US=> MkTzV2FPT0WU
human NB1 cell NY\1bJJOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVPJcohq[mm2aX;uJI9nKGi3bXHuJG5DOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwOU[xNVch|ryP M1HBXHNCVkeHUh?=
human MDA-MB-435 cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 MoHTOFghcA>? NHjFOGRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{WgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiR1m9NkDPxE1? M1q2UVIzPTZyNkK3
human MCF7 cells M{f5eHBzd2yrZnXyZZRqd25iYYPzZZk> NUDx[Y5tPDhiaB?= M2f5Z2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB2ODDodpMh[nliU2LCJIF{e2G7LDDHTVUxRTJizszN MnTYNlI2PjB4Mke=
human A549 cells MonNR5l1d3SxeHnjxsBie3OjeR?= MVK3NkBp MkfHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVIvPDRizszN Mo\BNlM3ODJ2NEG=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
Methods Test Index PMID
Western blot
p-AKT / AKT / p-ERK / ERK ; 

PubMed: 24759734     


Effect of 72 h treatment with sunitinib on SH-SY5Y, SK N BE(2), SK-N-AS and IMR-32 NB cell lines analyzed by Western blot with pSer(473)Akt, Akt, pThr202/Thr204 Erk1/2 and Erk1/2 antibodies. β-actin was used as a loading control.

p-GSK3β / GSK3β / MYCN ; 

PubMed: 24759734     


Effect of sunitinib on GSK3β phosphorylation and on MYCN total protein in MYCN amplified NB cell lines.

p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 19244102     


Sunitinib reduced Stat3 and Src activity, with no dramatic reduction of AKT, MAPK and JAK signaling in 786-O cells. Tumor cells were treated with sunitinib at indicated concentrations for 2 h (left panels) or 24 h (right panels). Total cell lysates were prepared and western blots were performed using relevant antibodies to detect total protein levels, with β-actin used as the loading control.

24759734 19244102
Growth inhibition assay
Cell viability; 

PubMed: 24369536     


Isolated effects of sunitinib malate on urinary bladder-cancer cell lines viability, assessed by using the MTT assay. The data shown and bars represent the mean values ± SD (SD: standard deviation). *P < 0.05 versus untreated cells.

24369536
体内試験 Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

Biochemical Tyrosine Kinase Assays:

IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferase fusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.
細胞試験:

[3]

+ 展開
  • 細胞株: RS4;11, MV4;11, and OC1-AML5
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間: 24 and 48 hours
  • 実験の流れ:

    Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.


    (参考用のみ)
動物試験:

[2]

+ 展開
  • 動物モデル: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • 製剤: Formulated as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution
  • 投薬量: ~80 mg/kg
  • 投与方法: Orally once daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 25 mg/mL (62.73 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5% DMSO+corn oil
混合させたのち直ちに使用することを推奨します。
7mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 398.47
化学式

C22H27FN4O2

CAS No. 557795-19-4
保管
in solvent
別名 SU11248

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04115189 Not yet recruiting Metastatic Renal Cell Carcinoma ( mRCC) Pfizer October 7 2019 --
NCT04033991 Not yet recruiting Carcinoma|Renal Cell Pfizer September 2019 --
NCT03900793 Recruiting Osteosarcoma University of Colorado Denver|National Cancer Institute (NCI) August 22 2019 Phase 1
NCT03846128 Not yet recruiting Metastatic Kidney Cancer University Hospital Rouen August 2019 --
NCT03905889 Suspended Renal Cell Carcinoma Metastatic Milton S. Hershey Medical Center|Eli Lilly and Company June 5 2019 Phase 1
NCT03916458 Not yet recruiting Carcinoma Renal Cell Pfizer April 18 2019 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

PDGFRシグナル伝達経路

相関PDGFR製品

Tags: Sunitinibを買う | Sunitinib ic50 | Sunitinib供給者 | Sunitinibを購入する | Sunitinib費用 | Sunitinib生産者 | オーダーSunitinib | Sunitinib化学構造 | Sunitinib分子量 | Sunitinib代理店
×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID